Delving into the Latest Updates on Oxetacaine with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Oxetacaine (INN), Oxethazaine (JP17/USAN), オキセサゼイン

+ [9]

Target-

Mechanism-

Therapeutic Areas

Nervous System DiseasesDigestive System DisordersMouth and Tooth Diseases+ [2]

Active Indication

Nausea and vomitingAnesthesiaGastroesophageal Reflux+ [1]

Inactive Indication

Esophagitis

Originator Organization

Alfresa Pharma Corp.

Active Organization

Alfresa Pharma Corp.

Inactive Organization

MEDA Pharma GmbH & Co. KG

Amato Pharmaceutical Products Ltd.

Drug Highest PhaseApproved

First Approval Date

JP (27 Feb 1962),

Nausea and vomiting

Regulation-

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Structure

Molecular FormulaC28H41N3O3

InChIKeyFTLDJPRFCGDUFH-UHFFFAOYSA-N

CAS Registry126-27-2

This is a randomised, double-blind, placebo-controlled, therapeutic confirmatory multicentre trial with 4 parallel treatment groups. The design is adaptive group-sequential with two interim analyses, possible sample size re-estimation after the first or second interim analysis and drop-the-loser approach. The study design was primarily chosen to show superior efficacy of Tepilta® compared to the single components and to placebo. Evaluation of safety is a secondary objective.

Start Date01 Apr 2011

Sponsor / Collaborator

MEDA Pharma GmbH & Co. KG

[+3]

EUCTR2009-014441-93-DE / Not yet recruitingPhase 3

Clinical trial to assess the efficacy of the fixed combination product Tepilta® in the treatment of radiation-induced oesophagitis compared to its active ingredients oxetacaine and antacids, and to placebo - Tepilta® vs. oxetacaine, antacids and placebo

Start Date16 Aug 2010

Sponsor / Collaborator

MEDA Pharma GmbH & Co. KG

100 Clinical Results associated with Oxetacaine

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100 Translational Medicine associated with Oxetacaine

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100 Patents (Medical) associated with Oxetacaine

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64

Literatures (Medical) associated with Oxetacaine

01 Oct 2021·Journal of Cellular BiochemistryQ3 · BIOLOGY

An integrated virtual screening and drug repurposing strategy for the discovery of new antimalarial drugs against Plasmodium falciparum phosphatidylinositol 3‐kinase

Q3 · BIOLOGY

Article

Author: Verma, Kanika ; Schneider, Kristan A. ; Bharti, Praveen K. ; Dubey, Shivangee ; Das, Aparup ; Verma, Anil K. ; Lahariya, Ayush K.

AbstractThe emergence and spread of drug resistance in Plasmodium falciparum, the parasite causing the most severe form of human malaria, is a major threat to malaria control and elimination programs around the globe. With P. falciparum having evolved widespread resistance against a number of previously widely used drugs, currently, artemisinin (ART) and its derivatives are the cornerstones of first‐line treatments of uncomplicated malaria. However, growing incidences of ART failure reflect the spread of ART‐resistant P. falciparum strains. Despite current efforts to understand the primary cause of ART resistance due to mutations in the Kelch 13 gene (PfK13), the mechanism underlying ART resistance is still not completely unclear and no feasible strategies to counteract the causes and thereby restoring the efficiency of ART have been developed. We use a polypharmacology approach to identify potential drugs that can be used for the novel purpose (target). Of note, we have designed a multimodal stratagem to identify approved drugs with a potential antimalarial activity using computational drug reprofiling. Our investigations suggest that oxetacaine, simvastatin, repaglinide, aclidinium, propafenone, and lovastatin could be repurposed for malaria control and prevention.

01 Jul 2020·Advanced BiosystemsQ3 · BIOLOGY

Parallelized Impedance‐Based Platform for Continuous Dose‐Response Characterization of Antischistosomal Drugs

Q3 · BIOLOGY

Article

Author: Lombardo, Flavio C. ; Dupuch, Matthias A. ; Keiser, Jennifer ; Modena, Mario M. ; Hierlemann, Andreas ; Ravaynia, Paolo S. ; Biendl, Stefan

AbstractSchistosomiasis is an acute and chronic disease caused by tropical parasitic worms of the genus Schistosoma, which parasitizes annually over 200 million people worldwide. Screening of antischistosomal compounds is hampered by the low throughput and potential subjectivity of the visual evaluation of the parasite phenotypes, which affects the current drug assays. Here, an impedance‐based platform, capable of assessing the viability of Schistosoma mansoni schistosomula exposed to drugs, is presented. This automated and parallelized platform enables unbiased and continuous measurements of dose–response relationships for more than 48 h. The platform performance is established by exposure of schistosomula to three test compounds, praziquantel, oxethazaine, and mefloquine, which are known to affect the larvae phenotypes. The system is thereafter used to investigate the response of schistosomula to methiothepine, an antipsychotic compound, which causes complex drug‐induced effects. Continuous monitoring of the parasites reveals transient behavioral phenotypes and allows for extracting temporal characteristics of dose–response curves, which are essential for selecting drugs that feature high activity and fast kinetics of action. These measurements demonstrate that impedance‐based detection provides a wealth of information for the in vitro characterization of candidate antischistosomals and, represents a promising tool for the identification of new lead compounds.

01 Jun 2017·Journal of Pharmacy and PharmacologyQ3 · MEDICINE

Complexation of oxethazaine with 2-hydroxypropyl-β-cyclodextrin: increased drug solubility, decreased cytotoxicity and analgesia at inflamed tissues

Q3 · MEDICINE

Article

Author: Volpato, Maria C ; Cabeça, Luís F ; Yokaichiya, Fabiano ; Prado, Andressa R ; Morais Gonçalves da Silva, Camila ; Franco, Margareth Kazuyo Kobayashi Dias ; de Paula, Eneida ; Oliveira-Nascimento, Laura ; Franz-Montan, Michelle

AbstractObjectivesOxethazaine (OXZ) is one of the few local anaesthetics that provides analgesia at low pH, but presents poor solubility, cytotoxicity and no parenteral formulations. To address these issues, we aimed to prepare OXZ host-guest inclusion complex with hydroxypropyl-beta-cyclodextrin (HP-β-CD).MethodsThe inclusion complex was formed by co-solubilization, followed by a job plot analysis to determine stoichiometry of complexation and dialysis equilibrium analysis (based on UV/VIS absorption and fluorescence profiles of OXZ). Complex formation was confirmed by phase-solubility data, X-ray, Scanning Electron Microscopy and DOSY-1H-NMR experiments. In vitro cytotoxicity was analysed by MTT test in 3T3 fibroblasts. In vivo analgesia was tested by Von Frey test (inflammatory wounds – rats).Key findingsOxethazaine complexed (1 : 1 molar ratio) with HP-β-CD, as indicated by loss of OZX crystalline structure (X-ray) and strong host: guest interaction (NMR, K = 198/m), besides increased solubility. In vitro cell survival improved with the complex (IC50 OXZ = 28.9 μm, OXZ : HP-β-CD = 57.8 μm). In addition, the complex (0.1% OXZ) promoted in vivo analgesia for the same time that 2% lidocaine/epinephrine did.ConclusionOur results show that complexation improved physicochemical and biological properties of OXZ, allowing its application to inflamed tissues by parenteral routes.

100 Deals associated with Oxetacaine

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External Link

KEGG	Wiki	ATC	Drug Bank
D01152	Oxetacaine	C05AD06	DB12532

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Nausea and vomiting	JP	Alfresa Pharma Corp.	27 Feb 1962
Anesthesia	-	-	-
Gastroesophageal Reflux	-	-	-
Pain	-	-	-

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Esophagitis	Phase 1	AT	MEDA Pharma GmbH & Co. KG	01 Apr 2011
Esophagitis	Phase 1	DE	MEDA Pharma GmbH & Co. KG	01 Apr 2011
Pain	Phase 1	JP	Amato Pharmaceutical Products Ltd.	-